Total synthesis of rapamycin.
- Ley, SV
- Tackett, MN
- Maddess, ML
- Anderson, JC
- Brennan, PE
- Cappi, MW
- Heer, JP
- Helgen, C
- Kori, M
- Kouklovsky, C
- Marsden, SP
- Norman, J
- Osborn, DP
- Palomero, MA
- Pavey, JB
- Pinel, C
- Robinson, LA
- Schnaubelt, J
- Scott, JS
- Spilling, CD
- Watanabe, H
- Wesson, KE
- Willis, MC
Publication date
January 2009
DOI Publisher
Wiley Journal
Chemistry - A European JournalAbstract
For over 30 years, rapamycin has generated a sustained and intense interest from the scientific community as a result of its exceptional pharmacological properties and challenging structural features. In addition to its well known therapeutic value as a potent immunosuppressive agent, rapamycin and its derivatives have recently gained prominence for the treatment of a wide variety of other human malignancies. Herein we disclose full details of our extensive investigation into the synthesis of rapamycin that culminated in a new and convergent preparation featuring a macro-etherification/catechol-templating strategy for construction of the macrocyclic core of this natural product
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